RET Inhibitors in Non-Small-Cell Lung Cancer - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/34503226/

RET rearrangements are observed in 1-2% of non-small-cell lung cancer (NSCLC) patients and result in the constitutive activation of downstream pathways normally implied in cell proliferation, growth, differentiation and survival....

Targeted Therapy for RET Fusion Lung Cancer: Breakthrough and Unresolved Issue - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/34497761/

Molecular drugs targeting mutated or rearranged oncogene drivers have become one of the standard recognized treatments in patients with advanced and recurrent non-small cell lung cancer. RET is located in...

Hallmarks of RET and Co-occuring Genomic Alterations in RET-aberrant Cancers - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/34493590/

doi: 10.1158/1535-7163.MCT-21-0329. Online ahead of print. 1 Department of Internal Medicine, University of South Florida, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL, USA. 2 H. Lee Moffitt...

ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/34450308/

SLCO1A/1B and CYP3A4 are unlikely to affect the pharmacokinetics of pralsetinib, but ABCG2 and especially ABCB1 markedly limit its brain and testis penetration, as well as oral availability. These effects...

Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/34402300/

Rearranged during transfection (RET) is a receptor tyrosine kinase essential for the normal development and maturation of a diverse range of tissues. Aberrant RET signaling in cancers, due to RET...